China's anti-AIDS new drug Serravino was approved for clinical trials

China News Service, Kunming, May 8 (Reporter Hu Yuanhang) The reporter learned from the Kunming Institute of Zoology, Chinese Academy of Sciences on the 8th that the new anti-AIDS drug Serravino, developed by the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, in 2019 On May 5, he obtained a clinical trial notice issued by the State Drug Administration of China and agreed to conduct clinical trials. The project is currently preparing for a Phase I clinical study. If the research and development is successful, it will better meet the clinical drug needs of the majority of AIDS patients.

According to reports, Serravino is China's first CCR5 receptor antagonist approved for clinical research. It has successively won the 13th Five-Year Plan for Major Technology Innovation, the Strategic Pilot Science and Technology Project of the Chinese Academy of Sciences, and the Independent Deployment of the Chinese Academy of Sciences. Funding for projects such as the Yunnan Science and Technology Department. Early basic research work was published in the world's leading journal Science and Medicinal Chemistry.

Researchers first designed a new structural type of CCR5 antagonist through computer-assisted drug design, using drug design strategies based on structure and metabolic pathways, and through multi-round structural modification and drug-optimization optimization of CCR5 antagonists through high-efficiency synthesis technology. The only crystal complex structure of the listed clinical drug, Maraviro and multiple CCR5 antagonists and CCR5 receptor, targeting CCR5 target, screening and researching the anti-HIV activity of CCR5 antagonists; Structural modification, pharmacodynamic evaluation and drug-optimization optimization, found a CCR5 antagonist drug candidate with a new skeleton - Serravino.

Preclinical studies have shown that compared with Maraviro, serrano has better antagonistic activity against CCR5 receptor, and has superior inhibitory activity and therapeutic index to various HIV strains, clinical strains and resistant strains. Malavino is equivalent or similar; but Serravin has good pharmacokinetic properties in rats and dogs, with little difference in species, no inhibition and induction of CYP450 enzyme, no potential drug-drug interaction, Good security.

Currently, Serravino and its series of compounds have been granted patents in the United States, Europe, Russia, South Korea and Australia.